{"corpus_id":20680558,"paper_sha":"6cf5d743cbf8186dfa7b636f8d4ebede4c36d768","doi":"10.1177/1087057110368294","arxiv_id":null,"pmid":20413646,"pmcid":"PMC4725312","mag_id":2160218408,"dblp_id":null,"acl_id":null,"title":"Development and Optimization of a High-Throughput Bioassay for TRPM7 Ion Channel Inhibitors","year":2010,"publication_date":"2010-04-22","venue":"Journal of biomolecular screening","journal":{"name":"Journal of Biomolecular Screening","pages":"498 - 507","volume":"15"},"journal_issn":null,"journal_title":null,"publication_types":["JournalArticle"],"pubmed_pub_types":["Journal Article","Research Support, N.I.H., Extramural"],"s2_fields_of_study":["Biology","Medicine","Chemistry"],"reference_count":33,"citation_count":27,"influential_citation_count":1,"is_open_access":true,"arxiv_categories":null,"arxiv_license":null,"arxiv_journal_ref":null,"mesh_headings":[{"d":"Animals","mj":false,"ui":"D000818"},{"d":"Cell Line","mj":false,"ui":"D002460"},{"d":"Fluorescent Dyes","mj":false,"qs":[{"q":"metabolism","mj":false,"ui":"Q000378"}],"ui":"D005456"},{"d":"Fura-2","mj":false,"qs":[{"q":"analogs & derivatives","mj":false,"ui":"Q000031"},{"q":"metabolism","mj":false,"ui":"Q000378"}],"ui":"D016257"},{"d":"High-Throughput Screening Assays","mj":false,"qs":[{"q":"methods","mj":true,"ui":"Q000379"},{"q":"standards","mj":false,"ui":"Q000592"}],"ui":"D057166"},{"d":"Humans","mj":false,"ui":"D006801"},{"d":"Magnesium","mj":false,"qs":[{"q":"metabolism","mj":false,"ui":"Q000378"}],"ui":"D008274"},{"d":"Manganese","mj":false,"qs":[{"q":"metabolism","mj":false,"ui":"Q000378"}],"ui":"D008345"},{"d":"Patch-Clamp Techniques","mj":false,"ui":"D018408"},{"d":"Poloxamer","mj":false,"qs":[{"q":"metabolism","mj":false,"ui":"Q000378"}],"ui":"D020442"},{"d":"Probenecid","mj":false,"qs":[{"q":"metabolism","mj":false,"ui":"Q000378"}],"ui":"D011339"},{"d":"Protein Serine-Threonine Kinases","mj":false,"ui":"D017346"},{"d":"Reproducibility of Results","mj":false,"ui":"D015203"},{"d":"Surface-Active Agents","mj":false,"qs":[{"q":"metabolism","mj":false,"ui":"Q000378"}],"ui":"D013501"},{"d":"TRPM Cation Channels","mj":false,"qs":[{"q":"antagonists & inhibitors","mj":true,"ui":"Q000037"}],"ui":"D050053"},{"d":"Uricosuric Agents","mj":false,"qs":[{"q":"metabolism","mj":false,"ui":"Q000378"}],"ui":"D014528"}],"chemicals":[{"n":"Fluorescent Dyes","ui":"D005456","reg":"0"},{"n":"Surface-Active Agents","ui":"D013501","reg":"0"},{"n":"TRPM Cation Channels","ui":"D050053","reg":"0"},{"n":"Uricosuric Agents","ui":"D014528","reg":"0"},{"n":"fura-2-am","ui":"C049925","reg":"105344-37-4"},{"n":"Poloxamer","ui":"D020442","reg":"106392-12-5"},{"n":"Manganese","ui":"D008345","reg":"42Z2K6ZL8P"},{"n":"Protein Serine-Threonine Kinases","ui":"D017346","reg":"EC 2.7.11.1"},{"n":"TRPM7 protein, human","ui":"C486583","reg":"EC 2.7.11.1"},{"n":"Magnesium","ui":"D008274","reg":"I38ZP9992A"},{"n":"Probenecid","ui":"D011339","reg":"PO572Z7917"},{"n":"Fura-2","ui":"D016257","reg":"TSN3DL106G"}],"comments_corrections":null,"source_flags":5,"s2_open_access_pdf_url":"https://journals.sagepub.com/doi/pdf/10.1177/1087057110368294","s2_open_access_landing_url":"https://www.semanticscholar.org/paper/6cf5d743cbf8186dfa7b636f8d4ebede4c36d768","s2_open_access_license":"CCBYNCND","s2_open_access_status":"HYBRID","pmc_open_access_pdf_url":null,"pmc_open_access_landing_url":null,"pmc_open_access_license":null,"pmc_open_access_status":null,"unpaywall_open_access_pdf_url":null,"unpaywall_open_access_landing_url":null,"unpaywall_open_access_license":null,"unpaywall_open_access_status":null,"abstract":"TRPM7 is a ubiquitously expressed and constitutively active divalent cation channel essential for cell survival and proliferation because it provides a mechanism for Mg2+ entry. 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The bioassay was validated by measuring the effects of the known (nonselective) inhibitor 2-APB and La3+ on Mn2+ influx, and furthermore, the performance of the assay was evaluated by screening a subset of a marine bacteria-derived extract library. 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